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Factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of neutral P1 substituents |
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| Authors: | Nazaré Marc Essrich Melanie Will David W Matter Hans Ritter Kurt Urmann Matthias Bauer Armin Schreuder Herman Dudda Angela Czech Jörg Lorenz Martin Laux Volker Wehner Volkmar |
| Affiliation: | Aventis Pharma Deutschland GmbH, D-65926 Frankfurt am Main, Germany. marc.nazare@aventis.com |
| Abstract: | A series of novel, highly potent 2-carboxyindole-based factor Xa inhibitors is described. Structural requirements for neutral ligands, which bind in the S1 pocket of factor Xa were investigated with the 2-carboxyindole scaffold. This privileged fragment assembly approach yielded a set of equipotent, selective inhibitors with structurally diverse neutral P1 substituents. |
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